Affinity-Based Fluorescence Polarization Assay for High-Throughput Screening of Prolyl Hydroxylase 2 Inhibitors

Yonghua Lei, Tianhan Hu, Xingsen Wu, Yue Wu, Qichao Bao, Lianshan Zhang, Hua Xia, Haopeng Sun, Qidong You, Xiaojin Zhang

Research output: Contribution to journalArticlepeer-review

22 Scopus citations

Abstract

Prolyl hydroxylase domain 2 (PHD2) enzyme, a FeII and 2-oxoglutarate (2-OG) dependent oxygenase, mediates key physiological responses to hypoxia by modulating the levels of hypoxia inducible factor 1-α (HIF1α). PHD2 has been shown to have the therapeutic potentials for conditions including anemia and ischemic disease. Currently, many activity-based assays have been developed for identifying PHD2 inhibitors. Here we report an affinity-based fluorescence polarization method using FITC-labeled HIF1α (556-574) peptide as a probe for quantitative and site-specific screening of small molecule PHD2 inhibitors.

Original languageEnglish (US)
Pages (from-to)1236-1240
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume6
Issue number12
DOIs
StatePublished - Dec 10 2015
Externally publishedYes

Keywords

  • FITC-labeled probe
  • PHD2
  • affinity-based
  • fluorescence polarization assay

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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